CR20220105A - BIFUNCTIONAL DEGRADATORS OF BRD9 AND THEIR METHODS OF USE - Google Patents

BIFUNCTIONAL DEGRADATORS OF BRD9 AND THEIR METHODS OF USE

Info

Publication number
CR20220105A
CR20220105A CR20220105A CR20220105A CR20220105A CR 20220105 A CR20220105 A CR 20220105A CR 20220105 A CR20220105 A CR 20220105A CR 20220105 A CR20220105 A CR 20220105A CR 20220105 A CR20220105 A CR 20220105A
Authority
CR
Costa Rica
Prior art keywords
brd9
degradators
bifunctional
methods
bromodomain protein
Prior art date
Application number
CR20220105A
Other languages
Spanish (es)
Inventor
Julien Lorber
Thomas Zoller
Edmund Martin Harrington
Anna Vulpetti
Martin Sendzik
Xin Chen
Gregory John Hollingworth
Marie-Line Goude
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CR20220105A publication Critical patent/CR20220105A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La divulgación proporciona compuestos bifuncionales para BRD9 de Fórmula (A), o una de sus sales, hidratos, solvatos, profármacos, estereoisómeros o tautómeros farmacéuticamente aceptables, su preparación, composiciones farmacéuticas que los comprenden, y su uso en el tratamiento de enfermedades y trastornos mediados por una proteína con bromodominio, tal como proteína con bromodominio 9 (BRD9).The disclosure provides bifunctional compounds for BRD9 of Formula (A), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer or tautomer thereof, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of diseases and disorders. mediated by a bromodomain protein, such as bromodomain protein 9 (BRD9).

CR20220105A 2019-09-16 2020-09-14 BIFUNCTIONAL DEGRADATORS OF BRD9 AND THEIR METHODS OF USE CR20220105A (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962900869P 2019-09-16 2019-09-16
US201962900860P 2019-09-16 2019-09-16
US201962900863P 2019-09-16 2019-09-16
US201962900865P 2019-09-16 2019-09-16
PCT/US2020/050768 WO2021055295A1 (en) 2019-09-16 2020-09-14 Brd9 bifunctional degraders and their methods of use

Publications (1)

Publication Number Publication Date
CR20220105A true CR20220105A (en) 2022-06-13

Family

ID=72915891

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220105A CR20220105A (en) 2019-09-16 2020-09-14 BIFUNCTIONAL DEGRADATORS OF BRD9 AND THEIR METHODS OF USE

Country Status (20)

Country Link
US (1) US20220315578A1 (en)
EP (1) EP4041724A1 (en)
JP (1) JP2022547952A (en)
KR (1) KR20220063192A (en)
CN (1) CN114641473A (en)
AU (1) AU2020349451B2 (en)
BR (1) BR112022003514A2 (en)
CA (1) CA3153529A1 (en)
CO (1) CO2022002842A2 (en)
CR (1) CR20220105A (en)
DO (1) DOP2022000053A (en)
EC (1) ECSP22018571A (en)
IL (1) IL290677A (en)
JO (1) JOP20220069A1 (en)
MX (1) MX2022003102A (en)
PE (1) PE20221417A1 (en)
PH (1) PH12022550611A1 (en)
TW (1) TW202123942A (en)
UY (1) UY38880A (en)
WO (1) WO2021055295A1 (en)

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* Cited by examiner, † Cited by third party
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EP3746135A4 (en) 2018-01-30 2022-03-09 Foghorn Therapeutics Inc. Methods and compounds for treating disorders
WO2020160198A1 (en) 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
US20230066136A1 (en) 2019-01-29 2023-03-02 Foghorn Therapeutics Inc. Compounds and uses thereof
US20220387602A1 (en) * 2019-09-16 2022-12-08 Novartis Ag Bifunctional degraders and their methods of use
TWI877297B (en) 2020-01-29 2025-03-21 美商福宏治療公司 Compounds and uses thereof
WO2021178920A1 (en) 2020-03-05 2021-09-10 C4 Therapeutics, Inc. Compounds for targeted degradation of brd9
US11787800B2 (en) 2020-07-29 2023-10-17 Foghorn Therapeutics Inc. BRD9 degraders and uses thereof
US11767330B2 (en) 2021-07-06 2023-09-26 Foghorn Therapeutics Inc. Citrate salt, pharmaceutical compositions, and methods of making and using the same
WO2023039208A1 (en) * 2021-09-09 2023-03-16 C4 Therapeutics, Inc. Selected compounds for targeted degradation of brd9
WO2023109892A1 (en) * 2021-12-15 2023-06-22 海思科医药集团股份有限公司 Compound for inhibiting or degrading brd9, and composition and pharmaceutical use thereof
WO2023200800A1 (en) * 2022-04-11 2023-10-19 Foghorn Therapeutics Inc. Methods of treating androgen receptor-independent prostate cancer
WO2024163609A1 (en) * 2023-02-01 2024-08-08 Foghorn Therapeutics Inc. Compositions for treating cancer
WO2024240840A1 (en) 2023-05-24 2024-11-28 Beactica Therapeutics Ab Aromatic amides and conjugates thereof as binders to tead
CN117229202B (en) * 2023-11-15 2024-01-26 苏州美诺医药科技有限公司 Preparation method of intermediate of BRD9 targeted degradation compound

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US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
CN107257800B (en) * 2014-12-23 2020-06-30 达纳-法伯癌症研究所股份有限公司 Method for inducing target protein degradation by bifunctional molecules
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2016139361A1 (en) * 2015-03-05 2016-09-09 Boehringer Ingelheim International Gmbh New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9
CA3025806C (en) * 2016-06-23 2023-04-04 Dana-Farber Cancer Institute, Inc. Degradation of bromodomain-containing protein 9 (brd9) by conjugation of brd9 inhibitors with e3 ligase ligand and methods of use
WO2018064589A1 (en) * 2016-09-29 2018-04-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation using a mutant e3 ubiquitin ligase
MX2019009046A (en) * 2017-01-31 2019-10-30 Arvinas Operations Inc Cereblon ligands and bifunctional compounds comprising the same.
US11065231B2 (en) * 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
JP2021506848A (en) * 2017-12-18 2021-02-22 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト E3 Bifunctional inhibitor with EGFR with ubiquitin ligase moiety
WO2019140387A1 (en) * 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
CN117186108A (en) * 2018-03-26 2023-12-08 诺华股份有限公司 Bruton's tyrosine kinase degrader
WO2019186343A1 (en) * 2018-03-26 2019-10-03 Novartis Ag N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
WO2020051235A1 (en) * 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
WO2020160198A1 (en) * 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2020160192A1 (en) * 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof

Also Published As

Publication number Publication date
PE20221417A1 (en) 2022-09-20
AU2020349451A1 (en) 2022-04-21
MX2022003102A (en) 2022-04-06
WO2021055295A1 (en) 2021-03-25
AU2020349451B2 (en) 2024-02-01
CO2022002842A2 (en) 2022-04-19
JP2022547952A (en) 2022-11-16
CA3153529A1 (en) 2021-03-25
DOP2022000053A (en) 2023-01-31
UY38880A (en) 2021-04-30
EP4041724A1 (en) 2022-08-17
BR112022003514A2 (en) 2022-05-17
KR20220063192A (en) 2022-05-17
IL290677A (en) 2022-04-01
PH12022550611A1 (en) 2023-03-13
JOP20220069A1 (en) 2023-01-30
US20220315578A1 (en) 2022-10-06
CN114641473A (en) 2022-06-17
ECSP22018571A (en) 2022-04-29
TW202123942A (en) 2021-07-01

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